EA023132B1 - Бициклические азагетероциклические карбоксамиды - Google Patents

Бициклические азагетероциклические карбоксамиды Download PDF

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Publication number
EA023132B1
EA023132B1 EA201300186A EA201300186A EA023132B1 EA 023132 B1 EA023132 B1 EA 023132B1 EA 201300186 A EA201300186 A EA 201300186A EA 201300186 A EA201300186 A EA 201300186A EA 023132 B1 EA023132 B1 EA 023132B1
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EA
Eurasian Patent Office
Prior art keywords
methyl
ethyl
methylamino
amino
azetidin
Prior art date
Application number
EA201300186A
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English (en)
Russian (ru)
Other versions
EA201300186A1 (ru
Inventor
Бейард Р. Хак
Константин Неагу
Рейнальдо С. Джонс
Лизбет Селест Деселм
Юфан Сяо
Сриниваса Р. Карра
Руокси Лань
Игорь Мочалкин
Аманда Э. Саттон
Томас Э. Ричардсон
Original Assignee
Мерк Патент Гмбх
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Application filed by Мерк Патент Гмбх filed Critical Мерк Патент Гмбх
Publication of EA201300186A1 publication Critical patent/EA201300186A1/ru
Publication of EA023132B1 publication Critical patent/EA023132B1/ru

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/86Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/94Nitrogen atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/74Quinazolines; Hydrogenated quinazolines with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, attached to ring carbon atoms of the hetero ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Dermatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
EA201300186A 2010-07-29 2011-07-01 Бициклические азагетероциклические карбоксамиды EA023132B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US36896410P 2010-07-29 2010-07-29
PCT/EP2011/003272 WO2012013282A1 (en) 2010-07-29 2011-07-01 Bicyclic azaheterocyclic carboxamides as inhibitors of the kinase p70s6k

Publications (2)

Publication Number Publication Date
EA201300186A1 EA201300186A1 (ru) 2013-12-30
EA023132B1 true EA023132B1 (ru) 2016-04-29

Family

ID=44532723

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201300186A EA023132B1 (ru) 2010-07-29 2011-07-01 Бициклические азагетероциклические карбоксамиды

Country Status (19)

Country Link
US (1) US8710044B2 (sr)
EP (1) EP2598492B1 (sr)
JP (1) JP5894157B2 (sr)
KR (1) KR101852644B1 (sr)
CN (1) CN103003250B (sr)
AR (1) AR082414A1 (sr)
AU (1) AU2011285247B2 (sr)
BR (1) BR112013002090A2 (sr)
CA (1) CA2806610C (sr)
CL (1) CL2013000263A1 (sr)
EA (1) EA023132B1 (sr)
ES (1) ES2557383T3 (sr)
HK (1) HK1183302A1 (sr)
IL (1) IL224072A (sr)
MX (1) MX2013001054A (sr)
NZ (1) NZ604379A (sr)
SG (1) SG187166A1 (sr)
UA (1) UA110113C2 (sr)
WO (1) WO2012013282A1 (sr)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8563573B2 (en) 2007-11-02 2013-10-22 Vertex Pharmaceuticals Incorporated Azaindole derivatives as CFTR modulators
US8802868B2 (en) 2010-03-25 2014-08-12 Vertex Pharmaceuticals Incorporated Solid forms of (R)-1(2,2-difluorobenzo[D][1,3]dioxo1-5-yl)-N-(1-(2,3-dihydroxypropyl-6-fluoro-2-(1-hydroxy-2-methylpropan2-yl)-1H-Indol-5-yl)-Cyclopropanecarboxamide
ES2858351T3 (es) 2010-04-22 2021-09-30 Vertex Pharma Compuesto intermedio para proceso de producción de compuestos de cicloalquilcaraboxamido-indol
WO2012016001A1 (en) * 2010-07-29 2012-02-02 Merck Patent Gmbh Cyclic amine azaheterocyclic carboxamides
EA023821B1 (ru) * 2010-11-24 2016-07-29 Мерк Патент Гмбх Хиназолинкарбоксамидазетидины, их применение в лечении гиперпролиферативных заболеваний и содержащие их композиции
JP5964974B2 (ja) 2011-09-12 2016-08-03 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングMerck Patent Gesellschaft mit beschraenkter Haftung キナーゼ活性のモジュレーターとしての新規イミダゾールアミン
CN103930407B (zh) 2011-09-12 2019-02-26 默克专利有限公司 用作激酶活性调节剂的氨基嘧啶衍生物
EP2920154B1 (en) 2012-11-16 2017-10-11 Merck Patent GmbH Novel imidazol-piperidinyl derivatives as modulators of kinase activity
US9580443B2 (en) 2012-11-16 2017-02-28 Merck Patent Gmbh Heterocyclic derivatives as modulators of kinase activity
ES2821102T3 (es) * 2012-11-29 2021-04-23 Merck Patent Gmbh Derivados de azaquinazolincarboxamida
SG10201900954SA (en) 2013-03-11 2019-02-27 Merck Patent Gmbh Heterocycles as Modulators of Kinase Activity
CN103232401B (zh) * 2013-04-12 2015-11-04 浙江工业大学 一种4-芳硫基喹唑啉类化合物的合成方法
CN103254141B (zh) * 2013-04-26 2016-02-24 浙江工业大学 4-[4-(2-二丙氨基乙酰氨基)苯胺基]-6-取代喹唑啉类化合物及制备和应用
SG11201608189WA (en) 2014-04-03 2016-10-28 Merck Patent Gmbh Combinations of cancer therapeutics
RU2744460C2 (ru) 2014-04-15 2021-03-09 Вертекс Фармасьютикалз Инкорпорейтед Фармацевтические композиции для лечения заболеваний, опосредованных муковисцидозным трансмембранным регулятором проводимости
JP2023522965A (ja) * 2020-04-21 2023-06-01 ユニバーシティ オブ マサチューセッツ 加齢性黄斑変性を処置するための方法および組成物
JP2023551408A (ja) 2020-11-16 2023-12-08 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング がん処置のためのキナーゼインヒビター組み合わせ
WO2023039068A1 (en) * 2021-09-08 2023-03-16 Neubase Therapeutics, Inc. Compositions and methods for synthesis of peptide nucleic acid intermediates

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004014861A1 (ja) * 2002-08-09 2004-02-19 Kyorin Pharmaceutical Co., Ltd. 4-置換キノリン-8-カルボン酸アミド誘導体とその薬理上許容される付加塩
WO2005120509A1 (en) * 2004-06-04 2005-12-22 Amphora Discovery Corporation Quinoline- and isoquinoline-based compounds exhibiting atp-utilizing enzyme inhibitory activity, and compositions, and uses thereof
WO2010093419A1 (en) * 2009-02-11 2010-08-19 Merck Patent Gmbh Novel amino azaheterocyclic carboxamides

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9613021D0 (en) * 1996-06-21 1996-08-28 Pharmacia Spa Bicyclic 4-aralkylaminopyrimidine derivatives as tyrosine kinase inhibitors
AR016817A1 (es) * 1997-08-14 2001-08-01 Smithkline Beecham Plc Derivados de fenilurea o feniltiourea, procedimiento para su preparacion, coleccion de compuestos, compuestos intermediarios, composicion farmaceutica,metodo de tratamiento y uso de dichos compuestos para la manufactura de un medicamento
DE60144322D1 (de) * 2000-04-27 2011-05-12 Astellas Pharma Inc Kondensierte heteroarylderivate
TW200306819A (en) 2002-01-25 2003-12-01 Vertex Pharma Indazole compounds useful as protein kinase inhibitors
WO2004014873A1 (ja) * 2002-08-09 2004-02-19 Kyorin Pharmaceutical Co., Ltd. 4-置換キナゾリン-8-カルボン酸アミド誘導体とその薬理上許容される付加塩
WO2004092154A1 (en) 2003-04-03 2004-10-28 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of protein kinases
EP1670771A4 (en) 2003-09-30 2010-09-01 Irm Llc COMPOUNDS AND COMPOSITIONS INHIBITING PROTEIN-KINASES
US7816353B2 (en) 2003-10-24 2010-10-19 Exelixis, Inc. P70S6 kinase modulators and method of use
ES2308272T3 (es) 2003-11-21 2008-12-01 Novartis Ag Derivados de 1h-imidazoquinolina como inhibidores de la proteina quinasa.
US8044057B2 (en) 2003-12-09 2011-10-25 The United States Of America As Represented By The Secretary Of The Department Of Health And Human Services Methods for suppressing an immune response or treating a proliferative disorder
US8076338B2 (en) 2004-04-23 2011-12-13 Exelixis, Inc. Kinase modulators and methods of use
EP1848719B1 (en) 2004-12-28 2012-02-01 Exelixis, Inc. [1h-pyrazolo[3,4-d]pyrimidin-4-yl]-piperidine or -piperazine compounds as serine-threonine kinase modulators (p70s6k, atk1 and atk2) for the treatment of immunological, inflammatory and proliferative diseases
GB0501999D0 (en) 2005-02-01 2005-03-09 Sentinel Oncology Ltd Pharmaceutical compounds
WO2006136821A1 (en) 2005-06-22 2006-12-28 Astex Therapeutics Limited Pharmaceutical compounds
UA99284C2 (ru) 2007-05-11 2012-08-10 Елі Ліллі Енд Компані ИНГИБИТОРЫ р70 S6-КИНАЗЫ

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004014861A1 (ja) * 2002-08-09 2004-02-19 Kyorin Pharmaceutical Co., Ltd. 4-置換キノリン-8-カルボン酸アミド誘導体とその薬理上許容される付加塩
WO2005120509A1 (en) * 2004-06-04 2005-12-22 Amphora Discovery Corporation Quinoline- and isoquinoline-based compounds exhibiting atp-utilizing enzyme inhibitory activity, and compositions, and uses thereof
WO2010093419A1 (en) * 2009-02-11 2010-08-19 Merck Patent Gmbh Novel amino azaheterocyclic carboxamides

Also Published As

Publication number Publication date
US20130137677A1 (en) 2013-05-30
MX2013001054A (es) 2013-02-21
BR112013002090A2 (pt) 2016-05-24
AU2011285247A1 (en) 2013-03-14
EP2598492B1 (en) 2015-10-28
CA2806610C (en) 2018-08-28
CN103003250A (zh) 2013-03-27
NZ604379A (en) 2015-01-30
AR082414A1 (es) 2012-12-05
JP2013532668A (ja) 2013-08-19
KR101852644B1 (ko) 2018-04-26
CL2013000263A1 (es) 2013-09-06
SG187166A1 (en) 2013-02-28
EA201300186A1 (ru) 2013-12-30
KR20130096714A (ko) 2013-08-30
US8710044B2 (en) 2014-04-29
CA2806610A1 (en) 2012-02-02
HK1183302A1 (zh) 2013-12-20
IL224072A0 (en) 2013-03-05
IL224072A (en) 2016-02-29
AU2011285247B2 (en) 2016-08-04
ES2557383T3 (es) 2016-01-25
WO2012013282A1 (en) 2012-02-02
WO2012013282A8 (en) 2012-03-29
JP5894157B2 (ja) 2016-03-23
CN103003250B (zh) 2016-02-17
UA110113C2 (xx) 2015-11-25
EP2598492A1 (en) 2013-06-05

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MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

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